Target Information

Target General Infomation
Target ID
T53381
Former ID
TTDS00030
Target Name
Alpha-1D adrenergic receptor
Gene Name
ADRA1D
Synonyms
Alpha 1D-adrenoceptor; Alpha 1D-adrenoreceptor; Alpha adrenergic receptor 1a; Alpha-1A adrenergic receptor; ADRA1D
Target Type
Successful
Disease Benign prostatic hyperplasia [ICD9: 600; ICD10: N40]
Congestive heart failure [ICD9: 428; ICD10: I50]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Erectile dysfunction [ICD9: 302.72, 607.84; ICD10: F52.2, N48.4]
Fecal incontinence [ICD10: R15]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Heart arrhythmia [ICD10: I47-I49]
Hypertension [ICD9: 401; ICD10: I10-I16]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Pediatric cancer [ICD9: 140-229; ICD10: C00-C96]
Prostate disease [ICD10: N42.9]
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9]
Prostate hyperplasia [ICD10: N40]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
Function
This alpha-adrenergic receptor mediatesits effect through the influx of extracellular calcium.
BioChemical Class
GPCR rhodopsin
Target Validation
T53381
UniProt ID
P25100
Sequence
MTFRDLLSVSFEGPRPDSSAGGSSAGGGGGSAGGAAPSEGPAVGGVPGGAGGGGGVVGAG
SGEDNRSSAGEPGSAGAGGDVNGTAAVGGLVVSAQGVGVGVFLAAFILMAVAGNLLVILS
VACNRHLQTVTNYFIVNLAVADLLLSATVLPFSATMEVLGFWAFGRAFCDVWAAVDVLCC
TASILSLCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWVVALVVSVGPLLGWKEPVP
PDERFCGITEEAGYAVFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGVKRERGKAS
EVVLRIHCRGAATGADGAHGMRSAKGHTFRSSLSVRLLKFSREKKAAKTLAIVVGVFVLC
WFPFFFVLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQ
CRRRRRRRPLWRVYGHHWRASTSGLRQDCAPSSGDAPPGAPLALTALPDPDPEPPGTPEM
QAPVASRRKPPSAFREWRLLGPFRRPTTQLRAKVSSLSHKIRAGGAQRAEAACAQRSEVE
AVSLGVPHEVAEGATCQAYELADYSNLRETDI
Drugs and Mode of Action
Drug(s) Alfuzosin Drug Info Approved Benign prostatic hyperplasia [536610], [542116]
Armodafinil Drug Info Approved Pediatric cancer [551871]
Bunazosin Drug Info Approved Glaucoma [551871]
Doxazosin Drug Info Approved Hypertension [536610], [542180]
Moxisylyte Drug Info Approved Erectile dysfunction [551871]
Phenylephrine hydrochloride gel Drug Info Approved Fecal incontinence [547809]
Terazosin Drug Info Approved Benign prostatic hyperplasia [538289], [542324]
Trimazosin Drug Info Approved Congestive heart failure [551871]
MEDETOMIDINE Drug Info Phase 2 Pain [529347]
DL-017 Drug Info Phase 1 Hypertension [526190]
INDORAMIN Drug Info Withdrawn from market Hypertension [468125], [551871]
Sunepitron Drug Info Discontinued in Phase 3 Discovery agent [545699]
TIOSPIRONE Drug Info Discontinued in Phase 3 Discovery agent [538617], [544679]
Dabuzalgron Drug Info Discontinued in Phase 2 Urinary incontinence [540407], [547205]
Deriglidole Drug Info Discontinued in Phase 2 Diabetes [544511]
FCE-22716 Drug Info Discontinued in Phase 2 Hypertension [533340]
FIDUXOSIN HYDROCHLORIDE Drug Info Discontinued in Phase 2 Prostate disease [547070]
GYKI-16084 Drug Info Discontinued in Phase 2 Prostate disease [546866]
JTH-601 Drug Info Discontinued in Phase 2 Prostate disease [546856]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [545274]
NS-49 Drug Info Discontinued in Phase 2 Urinary incontinence [468041], [545984]
OPC-28326 Drug Info Discontinued in Phase 2 Peripheral vascular disease [546957]
REC-15-2739 Drug Info Discontinued in Phase 2 Prostate disease [545508]
SL-25.1039 Drug Info Discontinued in Phase 2 Urinary incontinence [547287]
SL-89.0591 Drug Info Discontinued in Phase 2 Prostate disease [545536]
SOU-001 Drug Info Discontinued in Phase 2 Urinary incontinence [547251]
SUN-9221 Drug Info Discontinued in Phase 1 Hypertension [546178]
ABANOQUIL Drug Info Terminated Discovery agent [544556]
AGN-193080 Drug Info Terminated Discovery agent [546437]
BMY-7378 Drug Info Terminated Discovery agent [543289], [544847]
CR-2991 Drug Info Terminated Hypertension [547727]
NIGULDIPINE Drug Info Terminated Discovery agent [468083], [545183]
Siramesine Drug Info Terminated Discovery agent [545008]
SK&F-104078 Drug Info Terminated Discovery agent [544626]
SK&F-104856 Drug Info Terminated Discovery agent [544924]
SL-91.0893 Drug Info Terminated Prostate hyperplasia [546240]
SNAP-5089 Drug Info Terminated Heart arrhythmia [468115], [546179]
WB-4101 Drug Info Terminated Discovery agent [468117], [545656]
Sunepitron Drug Info Investigative Unspecified [528210]
Inhibitor (+/-)-nantenine Drug Info [530558]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [534315]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [534315]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl Drug Info [533509]
1-(2-Chloro-phenyl)-piperazine Drug Info [528039]
1-(2-Methoxy-phenyl)-piperazine Drug Info [528039]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine Drug Info [533509]
1-(pyridin-2-yl)piperazine Drug Info [533509]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Drug Info [526618]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info [534160]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info [534160]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info [533805]
4-(1-Naphthalen-1-yl-propyl)-1H-imidazole Drug Info [534160]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole Drug Info [534160]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole Drug Info [534160]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline Drug Info [526618]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol Drug Info [526729]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-(4-chlorobenzyl)-2-allylphthalazin-1(2H)-one Drug Info [528062]
4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one Drug Info [528062]
4-(4-chlorobenzyl)phthalazin-1(2H)-one Drug Info [528062]
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol Drug Info [526729]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info [534467]
4-Benzo[b]thiophen-4-yl-1H-imidazole Drug Info [525720]
4-benzyl-2-methylphthalazin-1(2H)-one Drug Info [528062]
4-Morpholin-2-yl-benzene-1,2-diol Drug Info [526729]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info [526778]
6-hydroxy-3-(3',5'-dihydroxyphenyl)coumarin Drug Info [527848]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info [526778]
ABANOQUIL Drug Info [533682]
AGN-192172 Drug Info [551280]
AGN-193080 Drug Info [551280]
BMY-7378 Drug Info [527512]
CORYNANTHEINE Drug Info [533638]
FLUANISONE Drug Info [533378]
Imidazolidin-2-ylidene-o-tolyl-amine Drug Info [551280]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine Drug Info [551280]
INDORAMIN Drug Info [533682]
ISOCLOZAPINE Drug Info [534532]
LEVONORDEFRIN Drug Info [534160]
MAZAPERTINE Drug Info [533800]
MEDETOMIDINE Drug Info [533805]
N-(5-Bromo-quinoxalin-6-yl)-guanidine Drug Info [551280]
NIGULDIPINE Drug Info [533638]
OCTOCLOTHEPIN Drug Info [531171]
RWJ-38063 Drug Info [525785]
RWJ-68157 Drug Info [525785]
RWJ-69736 Drug Info [525785]
RX-821002 Drug Info [533375]
Siramesine Drug Info [533739]
SK&F-104078 Drug Info [533638]
SK&F-104856 Drug Info [533638]
SK&F-105854 Drug Info [533638]
SK&F-106686 Drug Info [533638]
SK&F-86466 Drug Info [533638]
SNAP-5089 Drug Info [533638]
SNAP-8719 Drug Info [527512]
Sunepitron Drug Info [528210]
TIOSPIRONE Drug Info [534093]
UH-301 Drug Info [534363]
WB-4101 Drug Info [533682]
Agonist 4-Methoxyamphetamine Drug Info [551380]
Armodafinil Drug Info [544068], [550911]
Dabuzalgron Drug Info [540407]
SL-25.1039 Drug Info [550220]
Antagonist Alfuzosin Drug Info [535396]
CR-2991 Drug Info [550128]
Doxazosin Drug Info [536929]
FIDUXOSIN HYDROCHLORIDE Drug Info [526250]
GYKI-16084 Drug Info [528199]
JTH-601 Drug Info [525752]
OPC-28326 Drug Info [525613]
Terazosin Drug Info [535079], [535647]
Modulator Bunazosin Drug Info [527544], [551871]
Deriglidole Drug Info [534576]
DL-017 Drug Info [526190]
FCE-22716 Drug Info [533340]
Moxisylyte Drug Info [534246], [551871]
NS-49 Drug Info [525556]
Phenylephrine hydrochloride gel Drug Info [527269]
REC-15-2739 Drug Info [534138]
SL-89.0591 Drug Info [525538]
SL-91.0893 Drug Info [551953]
SOU-001 Drug Info [527154]
SUN-9221 Drug Info [525435]
Trimazosin Drug Info [533525], [551871]
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
Adrenergic signaling in cardiomyocytes
Vascular smooth muscle contraction
Salivary secretion
NetPath Pathway IL2 Signaling Pathway
Reactome Adrenoceptors
G alpha (q) signalling events
G alpha (12/13) signalling events
WikiPathways Monoamine GPCRs
Calcium Regulation in the Cardiac Cell
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 468041(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 481).
Ref 468083(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 487).
Ref 468115(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 498).
Ref 468117(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 499).
Ref 468125(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 501).
Ref 526190Antihypertensive action and blockade of alpha1-adrenoceptors by DL-017, a quinazoline derivative. J Cardiovasc Pharmacol. 2001 Dec;38(6):893-9.
Ref 528210J Med Chem. 2006 Jun 1;49(11):3116-35.An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Ref 529347Sedative and cardiopulmonary effects of medetomidine hydrochloride and xylazine hydrochloride and their reversal with atipamezole hydrochloride in calves. Am J Vet Res. 2008 Mar;69(3):319-29.
Ref 533340Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat. Pharmacology. 1989;38(2):78-92.
Ref 536610Alpha blockers for the treatment of benign prostatic hyperplasia. Rev Urol. 2007 Fall;9(4):181-90.
Ref 538289FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074823.
Ref 538617(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 101).
Ref 540407(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3469).
Ref 542116(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7109).
Ref 542180(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7170).
Ref 542324(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7302).
Ref 543289(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 9).
Ref 544511Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000010)
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Ref 525613Mechanisms of action of OPC-28326, a selective hindlimb vasodilator. J Pharmacol Exp Ther. 1999 Nov;291(2):604-11.
Ref 525720J Med Chem. 2000 Mar 9;43(5):765-8.alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
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Ref 526250Effect of fiduxosin, an antagonist selective for alpha(1A)- and alpha(1D)-adrenoceptors, on intraurethral and arterial pressure responses in conscious dogs. J Pharmacol Exp Ther. 2002 Feb;300(2):487-94.
Ref 526618Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
Ref 526729J Med Chem. 1992 Mar 20;35(6):1009-18.Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.
Ref 526778J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.
Ref 527154Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83.
Ref 527269Effects of topically instilled bunazosin, an alpha1-adrenoceptor antagonist, on constrictions induced by phenylephrine and ET-1 in rabbit retinal arteries. Invest Ophthalmol Vis Sci. 2004 Nov;45(11):4041-8.
Ref 527512J Med Chem. 2005 Apr 21;48(8):3076-9.Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
Ref 527544Bunazosin, a selective alpha1-adrenoceptor antagonist, as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage. Cardiovasc Drug Rev. 2005 Spring;23(1):43-56.
Ref 527848Bioorg Med Chem Lett. 2006 Jan 15;16(2):257-61. Epub 2005 Nov 3.Design, synthesis, and vasorelaxant and platelet antiaggregatory activities of coumarin-resveratrol hybrids.
Ref 528039J Med Chem. 1991 Jun;34(6):1850-4.Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
Ref 528062Bioorg Med Chem Lett. 2006 May 15;16(10):2786-90. Epub 2006 Mar 2.Vasorelaxant activity of phthalazinones and related compounds.
Ref 528199A novel approach to the treatment of benign prostatic hyperplasia. BJU Int. 2006 Jun;97(6):1252-5.
Ref 528210J Med Chem. 2006 Jun 1;49(11):3116-35.An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531171J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for |A(1)-adrenoceptors.
Ref 533340Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat. Pharmacology. 1989;38(2):78-92.
Ref 533375J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
Ref 533378J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
Ref 533509J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.
Ref 533525The hypotensive effect of trimazosin is not caused solely by alpha 1-adrenoceptor blockade. J Cardiovasc Pharmacol. 1984 Jan-Feb;6(1):142-50.
Ref 533638J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ref 533682J Med Chem. 1995 Sep 1;38(18):3415-44.Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Ref 533739J Med Chem. 1995 May 26;38(11):1998-2008.Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
Ref 533800J Med Chem. 1994 Apr 15;37(8):1060-2.A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Ref 533805J Med Chem. 1994 Jul 22;37(15):2328-33.A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.
Ref 534093J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
Ref 534138Functional antagonistic activity of Rec 15/2739, a novel alpha-1 antagonist selective for the lower urinary tract, on noradrenaline-induced contraction of human prostate and mesenteric artery. J Pharmacol Exp Ther. 1996 Jun;277(3):1237-46.
Ref 534160J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Ref 534246Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses. Eur J Clin Pharmacol. 1996;49(5):411-5.
Ref 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
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